1-(4-Aminophenoxy)-3-(dimethylamino)propan-2-ol → 2-[4-(3-Dimethylamino-2-hydroxy-propoxy)-phenylamino]-8-indan-5-yl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester

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Reaction Steps

Using the procedure outlined in Example 1(g) the title compound was prepared from 1-(4-amino-phenoxy)-3-dimethylamino-propan-2-ol (18 mg, 0.083 mmol) and 8-indan-5-yl-2-methanesulfonyl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester (from Example 1(e) above, 34 mg, 0.083 mmol). 3.1 mg of 2-[4-(3-dimethylamino-2-hydroxy-propoxy)-phenylamino]-8-indan-5-yl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester was obtained as a yellow solid. 1H NMR (300 MHz, CDCl3) δ (ppm): 9.38 (s, 1H), 8.52 (s, 1H), 7.50 (br, 1H), 7.40 (d, 2H), 7.28 (m, 3H), 7.19 (d, 1H), 6.66 (br, 2H), 4.40 (q, 2H), 4.05 (m, 1H), 3.90 (d, 2H), 3.10 (m, 4H), 2.52 (dd, 1H), 2.33 (m, 7H), 2.22 (m, 2H), 1.40 (t, 3H). Mass Spectrum (LCMS, ESI pos.) Calcd. For C30H33N5O5: 544.25 (M+H), Found: 544.4.

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